AU2016209349B2 - Compounds and methods for the targeted degradation of the Androgen Receptor - Google Patents

Compounds and methods for the targeted degradation of the Androgen Receptor Download PDF

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AU2016209349B2
AU2016209349B2 AU2016209349A AU2016209349A AU2016209349B2 AU 2016209349 B2 AU2016209349 B2 AU 2016209349B2 AU 2016209349 A AU2016209349 A AU 2016209349A AU 2016209349 A AU2016209349 A AU 2016209349A AU 2016209349 B2 AU2016209349 B2 AU 2016209349B2
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optionally substituted
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halo
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AU2016209349A1 (en
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Xin Chen
Andrew P. Crew
Hanqing Dong
Caterina Ferraro
Meizhong Jin
Yimin Qian
Kam Siu
Jing Wang
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Arvinas Inc
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Arvinas Inc
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Priority to AU2021257970A priority patent/AU2021257970A1/en
Priority to AU2023285742A priority patent/AU2023285742A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Psychiatry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Secondary Cells (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Lubricants (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Developing Agents For Electrophotography (AREA)
AU2016209349A 2015-01-20 2016-01-20 Compounds and methods for the targeted degradation of the Androgen Receptor Active AU2016209349B2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2020213376A AU2020213376B2 (en) 2015-01-20 2020-08-07 Compounds and methods for the targeted degradation of the androgen receptor
AU2021257970A AU2021257970A1 (en) 2015-01-20 2021-10-27 Compounds and methods for the targeted degradation of androgen receptor
AU2023285742A AU2023285742A1 (en) 2015-01-20 2023-12-19 Compounds and methods for the targeted degradation of androgen receptor

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562105210P 2015-01-20 2015-01-20
US62/105,210 2015-01-20
PCT/US2016/014187 WO2016118666A1 (en) 2015-01-20 2016-01-20 Compounds and methods for the targeted degradation of the androgen receptor

Related Child Applications (1)

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AU2020213376A Division AU2020213376B2 (en) 2015-01-20 2020-08-07 Compounds and methods for the targeted degradation of the androgen receptor

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AU2016209349A1 AU2016209349A1 (en) 2017-08-10
AU2016209349B2 true AU2016209349B2 (en) 2020-05-07

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AU2016209349A Active AU2016209349B2 (en) 2015-01-20 2016-01-20 Compounds and methods for the targeted degradation of the Androgen Receptor
AU2020213376A Active AU2020213376B2 (en) 2015-01-20 2020-08-07 Compounds and methods for the targeted degradation of the androgen receptor
AU2021257970A Abandoned AU2021257970A1 (en) 2015-01-20 2021-10-27 Compounds and methods for the targeted degradation of androgen receptor
AU2023285742A Pending AU2023285742A1 (en) 2015-01-20 2023-12-19 Compounds and methods for the targeted degradation of androgen receptor

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AU2020213376A Active AU2020213376B2 (en) 2015-01-20 2020-08-07 Compounds and methods for the targeted degradation of the androgen receptor
AU2021257970A Abandoned AU2021257970A1 (en) 2015-01-20 2021-10-27 Compounds and methods for the targeted degradation of androgen receptor
AU2023285742A Pending AU2023285742A1 (en) 2015-01-20 2023-12-19 Compounds and methods for the targeted degradation of androgen receptor

Country Status (11)

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US (3) US11352351B2 (de)
EP (1) EP3247708A4 (de)
JP (3) JP6817962B2 (de)
KR (5) KR20220029783A (de)
CN (1) CN107428734A (de)
AU (4) AU2016209349B2 (de)
BR (1) BR112017015497A2 (de)
CA (1) CA2974367A1 (de)
HK (2) HK1245791A1 (de)
MX (2) MX2017009454A (de)
WO (1) WO2016118666A1 (de)

Families Citing this family (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117736134A (zh) 2012-01-12 2024-03-22 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN107428734A (zh) 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
GB201504314D0 (en) * 2015-03-13 2015-04-29 Univ Dundee Small molecules
CA2979070A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
MX2018000360A (es) * 2015-07-10 2018-06-11 Arvinas Inc Moduladores basados en mdm2 de proteolisis y metodos de uso asociados.
EP3331906A1 (de) 2015-08-06 2018-06-13 Dana-Farber Cancer Institute, Inc. Einstellbarer endogener proteinabbau
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US9963433B2 (en) * 2016-01-29 2018-05-08 Wayne State University Anticancer drugs including the chemical structures of an androgen receptor ligand and a histone deacetylase inhibitor
CN109475528B (zh) 2016-04-22 2022-01-11 达纳-法伯癌症研究所股份有限公司 用于egfr降解的双功能分子和使用方法
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
EP3455219A4 (de) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. Amingebundene c3-glutarimiddegronimere für zielproteinabbau
GB2554071A (en) * 2016-09-14 2018-03-28 Univ Dundee Small molecules
EP3512842B1 (de) 2016-09-15 2024-01-17 Arvinas, Inc. Indolderivate als abbauer des östrogenrezeptors
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
JP7097880B2 (ja) * 2016-11-01 2022-07-08 コーネル ユニバーシティー Ｍａｌｔ１分解のための化合物
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
EP3559002A4 (de) 2016-12-23 2021-02-17 Arvinas Operations, Inc. Auf egfr-proteolyse gerichtete chimäre moleküle und zugehörige verfahren zur verwendung
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
JP2020504741A (ja) 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
WO2018140809A1 (en) 2017-01-26 2018-08-02 Arvinas, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
EP3577109A4 (de) * 2017-01-31 2020-11-18 Arvinas Operations, Inc. Cereblonliganden und bifunktionale verbindungen damit
JP7227912B2 (ja) 2017-02-08 2023-02-24 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド キメラ抗原受容体の調節
WO2018200981A1 (en) 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
CA3062161A1 (en) 2017-05-01 2018-11-08 Spg Therapeutics, Inc. Tripartite androgen receptor eliminators, methods and uses thereof
CN108976278B (zh) * 2017-06-05 2021-04-06 海创药业股份有限公司 一种嵌合分子及其制备和应用
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
IL271587B2 (en) 2017-06-22 2024-05-01 Catalyst Biosciences Inc Modified membrane-type serine protease 1 polypeptides (MTSP-1) and methods of use
CN111212835A (zh) * 2017-07-28 2020-05-29 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
CN111278815B (zh) 2017-09-04 2024-03-08 C4医药公司 戊二酰亚胺
KR20200090747A (ko) 2017-09-12 2020-07-29 에이전시 포 사이언스, 테크놀로지 앤드 리서치 이소프레닐시스테인 카복실 메틸트랜스퍼라제의 억제제로 유용한 화합물
IL295603B2 (en) 2017-09-22 2024-03-01 Kymera Therapeutics Inc Protein compounds and their uses
EP3684366A4 (de) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. Crbn-liganden und verwendungen davon
EP3710002A4 (de) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. Degrader und degrone für gezielten proteinabbau
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
CN107987055A (zh) * 2017-12-19 2018-05-04 刘秀云 硫代咪唑二酮类雄激素受体拮抗剂及其用途
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc IRAK joints and used in them
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
WO2019148055A1 (en) 2018-01-26 2019-08-01 Yale University Imide-based modulators of proteolysis and methods of use
WO2019191112A1 (en) 2018-03-26 2019-10-03 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
BR112020020196A2 (pt) * 2018-04-01 2021-01-26 Arvinas Operations, Inc. compostos que visam brm e métodos de uso associados
AU2019249231B2 (en) 2018-04-04 2022-04-21 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
WO2019218904A1 (zh) * 2018-05-18 2019-11-21 四川科伦博泰生物医药股份有限公司 非天然氨基酸类衍生物、其制备方法及用途
EP3578561A1 (de) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiroverbindungen
CN110684046B (zh) * 2018-07-06 2023-05-12 江苏恒瑞医药股份有限公司 一种新的咪唑啉类衍生物的制备方法
EP3817748A4 (de) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. Tricyclische crbn-liganden und verwendungen davon
CN110746399B (zh) * 2018-07-23 2022-04-22 上海美志医药科技有限公司 具有降解雄激素受体活性的化合物
EP3831811A4 (de) 2018-07-31 2022-04-20 Fimecs, Inc. Heterocyclische verbindung
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
EP3886904A4 (de) 2018-11-30 2022-07-13 Kymera Therapeutics, Inc. Irak-degrader und verwendungen davon
EP3886854A4 (de) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrol- und pyrazolverbindungen und verfahren zu deren verwendung
CN109762045A (zh) * 2018-12-14 2019-05-17 中山大学附属第一医院 一种双靶点构建protac的方法及其用途
CN113453681B (zh) 2018-12-19 2024-10-11 细胞基因公司 经取代的3-((3-氨基苯基)氨基)哌啶-2，6-二酮化合物、其组合物及使用它们的治疗方法
MX2021007475A (es) 2018-12-19 2021-08-05 Celgene Corp Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos.
EP3897631A4 (de) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. Gezielter proteinabbau
US20220081435A1 (en) * 2019-01-03 2022-03-17 The Regents Of The University Of Michigan Androgen receptor protein degraders
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2020160295A1 (en) 2019-01-30 2020-08-06 Montelino Therapeutics, Llc Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2020198055A1 (en) * 2019-03-22 2020-10-01 Yale University Allosteric bcr-abl proteolysis targeting chimeric compounds
AU2020253633A1 (en) 2019-04-05 2021-11-04 Kymera Therapeutics, Inc. STAT degraders and uses thereof
US20220241424A1 (en) 2019-04-16 2022-08-04 Northwestern University Treatment of cancer
KR20220004100A (ko) * 2019-04-18 2022-01-11 하이노바 파마슈티컬스 인코포레이티드 안드로겐 수용체를 표적 분해하는 이중 기능성의 키메라 헤테로 고리 화합물 및 이의 용도
GB201906705D0 (en) 2019-05-13 2019-06-26 Phoremost Ltd Methods
MX2021013774A (es) 2019-05-14 2021-12-10 Nuvation Bio Inc Compuestos anticancerigenos dirigidos a los receptores hormonales nucleares.
US20220257774A1 (en) * 2019-05-17 2022-08-18 Hinova Pharmaceuticals Inc. Aromatic amine ar ahd bet targeting protein degradation chimera compound and use
AU2020302118A1 (en) 2019-06-28 2022-02-24 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN112390852B (zh) * 2019-08-14 2022-10-18 上海济煜医药科技有限公司 作为蛋白降解剂的化合物及其制备方法和应用
CN112457367B (zh) * 2019-09-06 2022-08-23 上海济煜医药科技有限公司 作为蛋白降解剂的连环类化合物及其制备方法和应用
CN118085015A (zh) * 2019-09-06 2024-05-28 江西济民可信集团有限公司 作为蛋白降解剂的并环类化合物及其制备方法和用途
CN112574278B (zh) * 2019-09-29 2024-08-23 江西济民可信集团有限公司 作为蛋白降解剂杂环类化合物及其制备方法和医药应用
US11952349B2 (en) 2019-11-13 2024-04-09 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CN110845348A (zh) * 2019-12-10 2020-02-28 苏州国匡医药科技有限公司 一种arv-110中间体的制备方法
EP4076524A4 (de) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. Irak-degrader und verwendungen davon
EP4076520A4 (de) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. Irak-degrader und verwendungen davon
CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
IL294225A (en) * 2019-12-23 2022-08-01 Shanghai Jemincare Pharmaceuticals Co Ltd Method of preparation of a protein-degrading agent compound and application
BR112022012410A2 (pt) 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
CN113149981B (zh) * 2020-01-22 2022-07-05 苏州德亘生物医药有限公司 一种降解雄激素受体的蛋白降解靶向嵌合体
WO2021178920A1 (en) 2020-03-05 2021-09-10 C4 Therapeutics, Inc. Compounds for targeted degradation of brd9
CN113387930B (zh) * 2020-03-11 2022-07-12 苏州开拓药业股份有限公司 一种双官能化合物及其制备方法和用途
BR112022018678A2 (pt) 2020-03-19 2022-11-01 Kymera Therapeutics Inc Degradadores de mdm2 e usos dos mesmos
EP4146642A1 (de) 2020-05-09 2023-03-15 Arvinas Operations, Inc. Verfahren zur herstellung einer bifunktionellen verbindung, ultrareine formen der bifunktionellen verbindung und dosierungsformen damit
WO2021231927A1 (en) * 2020-05-14 2021-11-18 The Regents Of The University Of Michigan Androgen receptor protein degraders with a tricyclic cereblon ligand
EP4153587A4 (de) * 2020-05-18 2024-06-12 Montelino Therapeutics, Inc. Bifunktionelle verbindungen und verfahren zur gezielten ubiquitinierung des androgenrezeptors
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
CN113801098B (zh) 2020-06-12 2023-05-30 上海济煜医药科技有限公司 酞嗪酮类化合物及其制备方法和医药用途
AR122726A1 (es) 2020-06-24 2022-09-28 Celgene Corp Compuestos de unión de cereblon, composiciones de los mismos, y métodos de tratamiento con los mismos
EP4171568A4 (de) * 2020-06-24 2024-07-24 Celgene Corp Cereblonbindende verbindungen, zusammensetzungen daraus und behandlungsverfahren damit
WO2021262810A1 (en) * 2020-06-24 2021-12-30 Celgene Corporation Cereblon binding compounds, compositions thereof, and methods of treatment therewith
CN114163444B (zh) * 2020-09-11 2023-07-14 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
CN114181277A (zh) * 2020-09-15 2022-03-15 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
CN113527273B (zh) * 2020-10-28 2023-08-22 中国药科大学 靶向泛素化降解hmgcr的化合物或其可药用的盐、制备方法及用途
CN114262319B (zh) * 2020-12-01 2023-05-05 南昌奥瑞药业有限公司 一类双功能分子、其制备方法及其应用
WO2022120355A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead degraders and uses thereof
JP7434265B2 (ja) * 2020-12-30 2024-02-20 財團法人工業技術研究院 アンドロゲン受容体結合分子およびその使用
WO2022152821A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
US11834458B2 (en) 2021-03-23 2023-12-05 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
US11986532B2 (en) 2021-04-16 2024-05-21 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
JP2024516024A (ja) 2021-05-03 2024-04-11 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物
CA3217417A1 (en) 2021-05-05 2022-11-10 Kevin M. Guckian Compounds for targeting degradation of bruton's tyrosine kinase
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
CN117580575A (zh) * 2021-06-17 2024-02-20 南京明德新药研发有限公司 戊二酰亚胺取代的异噁唑稠环化合物及其应用
CN117561249A (zh) * 2021-06-25 2024-02-13 细胞基因公司 Cereblon结合化合物、其组合物及其用于治疗的方法
EP4359406A1 (de) * 2021-06-25 2024-05-01 Celgene Corporation Cereblonbindende verbindungen, zusammensetzungen daraus und behandlungsverfahren damit
JP2024525580A (ja) 2021-07-07 2024-07-12 バイオジェン・エムエイ・インコーポレイテッド Ｉｒａｋ４タンパク質の分解をターゲティングするための化合物
IL309941A (en) 2021-07-07 2024-03-01 Biogen Ma Inc Compounds to target degradation of IRAK4 proteins
CN115772210A (zh) * 2021-09-08 2023-03-10 苏州开拓药业股份有限公司 硫代乙内酰脲化合物或其药用盐的无定形物、晶体、药物组合物、制备方法和用途
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023039601A1 (en) * 2021-09-13 2023-03-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2023054549A1 (ja) 2021-09-30 2023-04-06 あすか製薬株式会社 分解誘導剤
KR20240111312A (ko) 2021-10-25 2024-07-16 카이메라 쎄라퓨틱스 인코포레이티드 Tyk2 분해제 및 이의 용도
WO2023093845A1 (zh) 2021-11-25 2023-06-01 江苏恒瑞医药股份有限公司 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用
WO2023147594A2 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TW202417425A (zh) 2022-06-27 2024-05-01 美商傳達治療有限公司 雌激素受體α降解劑及其使用方法
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
WO2024037616A1 (zh) * 2022-08-19 2024-02-22 正大天晴药业集团股份有限公司 包含环己基的化合物
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
WO2024064358A1 (en) 2022-09-23 2024-03-28 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
WO2024073507A1 (en) 2022-09-28 2024-04-04 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
WO2024165050A1 (en) * 2023-02-10 2024-08-15 Aubrak Therapeutics Proteolysis-targeting chimera (protac) compounds and uses thereof field

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015000867A1 (en) * 2013-07-03 2015-01-08 Glaxosmithkline Intellectual Property Development Limited Benzothiophene derivatives as estrogen receptor inhibitors

Family Cites Families (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ304569B6 (cs) 1996-07-24 2014-07-09 Celgene Corporation 1,3-Dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindolin pro použití pro snížení nežádoucí hladiny TNFα u savce
DE69841549D1 (de) 1997-05-14 2010-04-22 Sloan Kettering Inst Cancer Verfahren und zubereitungen zur zerstörung bestimmter proteine
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
JP2002543129A (ja) 1999-05-05 2002-12-17 メルク エンド カムパニー インコーポレーテッド 抗微生物剤としての新規なプロリン類
CZ20024214A3 (cs) 2000-06-28 2003-04-16 Bristol-Myers Squibb Company Selektivní androgen receptorový modulátor, způsob jeho identifikace, jeho konstrukce a použití
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
EP1322750A4 (de) 2000-09-08 2004-09-29 California Inst Of Techn Auf proteolyse gerichtetes chimäres pharmazeutikum
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
WO2002066512A1 (en) 2001-02-16 2002-08-29 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
TWI263640B (en) 2001-12-19 2006-10-11 Bristol Myers Squibb Co Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US20060128632A1 (en) 2002-07-02 2006-06-15 Sharma Sushil K Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
EP1651595A2 (de) 2003-05-30 2006-05-03 Rigel Pharmaceuticals, Inc. Ubiquitinligaseinhibitoren
US7932382B2 (en) 2004-01-16 2011-04-26 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
WO2005094818A1 (en) 2004-03-23 2005-10-13 Genentech, Inc. Azabicyclo-octane inhibitors of iap
SG152225A1 (en) 2004-04-07 2009-05-29 Novartis Ag Inhibitors of iap
US7244851B2 (en) 2004-07-02 2007-07-17 Genentech, Inc. Inhibitors of IAP
BRPI0513020A (pt) 2004-07-08 2008-04-22 Warner Lambert Co moduladores de andrÈgenio, seus usos, composição farmacêutica, formulação farmacêutica tópica e artigo de fabricação
TW200621723A (en) * 2004-09-09 2006-07-01 Chugai Pharmaceutical Co Ltd Novel imidazolidine derivative and use thereof
DK1836201T4 (da) 2004-12-20 2013-11-11 Genentech Inc Pyrrolidininhibitorer af IAP.
CN103083644B (zh) 2005-02-25 2014-05-28 泰特拉洛吉克药业公司 Iap二聚体抑制剂
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
WO2006113942A2 (en) 2005-04-20 2006-10-26 Schering Corporation Method of inhibiting cathepsin activity
ES2434946T3 (es) 2005-08-31 2013-12-18 Celgene Corporation Compuestos de isoindol imida y composiciones que los comprenden y métodos para usarlo
KR20080095895A (ko) 2006-03-03 2008-10-29 노파르티스 아게 Ｎ―포르밀 히드록실아민 화합물
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
MX2008012492A (es) 2006-03-29 2008-12-12 Univ California Compuestos de diariltiohidantoina.
KR101071516B1 (ko) 2006-05-05 2011-10-10 더 리젠츠 오브 더 유니버시티 오브 미시간 2가 ｓｍａｃ 모방체 및 그의 용도
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
US20100056495A1 (en) 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
CA2660806C (en) 2006-08-30 2015-06-16 Celgene Corporation 5-substituted isoindoline compounds
RU2448101C2 (ru) 2006-08-30 2012-04-20 Селджин Корпорейшн 5-замещенные изоиндолиновые соединения
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
WO2008109057A1 (en) 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
MX2009010667A (es) 2007-04-12 2010-02-24 Joyant Pharmaceuticals Inc Dimeros y trimeros mimeticos de smac utiles como agentes anti-cancer.
CA2683318C (en) 2007-04-13 2012-10-30 The Regents Of The University Of Michigan Diazo bicyclic smac mimetics and the uses thereof
NZ580226A (en) 2007-04-30 2012-11-30 Genentech Inc Dimer compounds as inhibitors of iap
WO2008144925A1 (en) 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
JP5282091B2 (ja) 2007-07-25 2013-09-04 ブリストル−マイヤーズ スクイブ カンパニー トリアジンキナーゼ阻害剤
JP2010535213A (ja) * 2007-07-31 2010-11-18 アンドロサイエンス コーポレーション アンドロゲン受容体分解（ａｒｄ）エンハンサーを含む組成物ならびに皮膚疾患および脱毛の予防的または治療的処理方法
EP2058312A1 (de) 2007-11-09 2009-05-13 Universita' degli Studi di Milano Mimetische SMAC-Verbindungen als Apoptoseinduktoren
KR101696938B1 (ko) 2008-10-29 2017-01-16 셀진 코포레이션 암의 치료에 사용하기 위한 이소인돌린 화합물
WO2010107485A1 (en) 2009-03-17 2010-09-23 The Trustees Of Columbia University In The City Of New York E3 ligase inhibitors
WO2010141805A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
EP2784076A1 (de) 2009-10-28 2014-10-01 Joyant Pharmaceuticals, Inc. Dimere SMAC-Mimetika
SI3202461T1 (sl) 2010-02-11 2019-05-31 Celgene Corporation Derivati arilmetoksi izoindolina in sestavki, ki jih vsebujejo in metode uporabe le teh
DK3124481T3 (en) 2010-02-16 2018-05-07 Aragon Pharmaceuticals Inc ANDROGEN RECEPTOR MODULATORS AND APPLICATIONS THEREOF
EP2588129A4 (de) 2010-06-30 2014-07-09 Univ Brandeis Auf kleine moleküle zielender proteinabbau
AU2011305315A1 (en) 2010-09-24 2013-03-28 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
AU2011338615B2 (en) 2010-12-07 2017-07-27 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
US8921378B2 (en) 2011-04-21 2014-12-30 Orion Corporation Androgen receptor modulating carboxamides
AU2012316055B2 (en) 2011-09-27 2016-05-12 Amgen Inc. Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer
WO2013071039A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
WO2013071035A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
CN117736134A (zh) 2012-01-12 2024-03-22 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
US20150119435A1 (en) 2012-05-11 2015-04-30 Yale University Compounds useful for promoting protein degradation and methods using same
WO2013175417A1 (en) 2012-05-24 2013-11-28 Novartis Ag Pyrrolopyrrolidinone compounds
CN107540594A (zh) 2012-05-30 2018-01-05 霍夫曼-拉罗奇有限公司 取代的吡咯烷‑2‑甲酰胺
WO2014011712A1 (en) 2012-07-10 2014-01-16 Bristol-Myers Squibb Company Iap antagonists
ES2742285T3 (es) 2012-07-31 2020-02-13 Novartis Ag Marcadores asociados con la sensibilidad a inhibidores del doble minuto humano 2 (MDM2)
EP2882740B1 (de) 2012-08-09 2017-03-01 Bristol-Myers Squibb Company Iap-antagonisten
ES2835248T3 (es) 2012-09-04 2021-06-22 Jiangsu Hengrui Medicine Co Derivados de imidazolina, métodos de preparación de los mismos y sus aplicaciones en medicina
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
WO2014047024A1 (en) 2012-09-18 2014-03-27 Bristol-Myers Squibb Company Iap antagonists
WO2014055461A1 (en) 2012-10-02 2014-04-10 Bristol-Myers Squibb Company Iap antagonists
CA2930030A1 (en) 2012-11-09 2014-05-15 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
AR094116A1 (es) 2012-12-20 2015-07-08 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de hdm2
EP2934535B1 (de) 2012-12-20 2017-07-19 Merck Sharp & Dohme Corp. Substituierte pyrrolopyrimidine als hdm2-inhibitoren
EP2752191A1 (de) 2013-01-07 2014-07-09 Sanofi Zusammensetzungen und Verfahren unter Verwendung von HDM2-Antagonisten und MEK-Hemmer
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
JP6266659B2 (ja) 2013-02-28 2018-01-24 アムジエン・インコーポレーテツド 癌の治療のための安息香酸誘導体ｍｄｍ２阻害剤
AU2014236812B2 (en) 2013-03-14 2018-03-01 Amgen Inc. Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
TW201534586A (zh) * 2013-06-11 2015-09-16 Orion Corp 新穎ｃｙｐ１７抑制劑／抗雄激素劑
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
WO2015006524A1 (en) 2013-07-12 2015-01-15 Bristol-Myers Squibb Company Iap antagonists
KR20170002446A (ko) * 2014-04-14 2017-01-06 아비나스 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
US20160022642A1 (en) 2014-07-25 2016-01-28 Yale University Compounds Useful for Promoting Protein Degradation and Methods Using Same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
CN107257800B (zh) 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 通过双功能分子诱导靶蛋白降解的方法
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN107428734A (zh) 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
CA2979070A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
MX2018000360A (es) 2015-07-10 2018-06-11 Arvinas Inc Moduladores basados en mdm2 de proteolisis y metodos de uso asociados.
WO2017011590A1 (en) 2015-07-13 2017-01-19 Arvinas, Inc. Alanine-based modulators of proteolysis and associated methods of use
WO2017024317A2 (en) 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3331906A1 (de) 2015-08-06 2018-06-13 Dana-Farber Cancer Institute, Inc. Einstellbarer endogener proteinabbau
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
KR20180097530A (ko) 2015-11-02 2018-08-31 예일 유니버시티 단백질분해 표적화 키메라 화합물(Proteolysis Targeting Chimera compound) 및 그의 제조 및 사용 방법
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
JP2020504741A (ja) 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015000867A1 (en) * 2013-07-03 2015-01-08 Glaxosmithkline Intellectual Property Development Limited Benzothiophene derivatives as estrogen receptor inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MOHLER, M.L. ET AL., "Androgen receptor antagonists: a patent review (2008 - 2011)", EXPERT OPINION ON THERAPEUTIC PATENTS, (2012), vol. 22, no. 5, doi:10.1517/13543776.2012.682571, ISSN 1354-3776, pages 541 - 565 *

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